Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization was written by Soares de Melo, Candice;Feng, Tzu-Shean;van der Westhuyzen, Renier;Gessner, Richard K.;Street, Leslie J.;Morgans, Garreth L.;Warner, Digby F.;Moosa, Atica;Naran, Krupa;Lawrence, Nina;Boshoff, Helena I. M.;Barry, Clifton E. III;Harris, C. John;Gordon, Richard;Chibale, Kelly. And the article was included in Bioorganic & Medicinal Chemistry in 2015.SDS of cas: 55661-33-1 This article mentions the following:
Whole-cell high-throughput screening of a diverse SoftFocus library against Mycobacterium tuberculosis (Mtb) generated a novel aminopyrazolo[1,5-a]pyrimidine hit series. The synthesis and structure activity relationship studies identified compounds with potent antimycobacterial activity. The SAR of over 140 compounds shows that the 2-pyridylmethylamine moiety at the C-7 position of the pyrazolopyrimidine scaffold was important for Mtb activity, whereas the C-3 position offered a higher degree of flexibility. The series was also profiled for in vitro cytotoxicity and microsomal metabolic stability as well as physicochem. properties. Consequently liabilities to be addressed in a future lead optimization campaign have been identified. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1SDS of cas: 55661-33-1).
Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.SDS of cas: 55661-33-1
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica